Bromoenol lactone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bromoenol lactone ((6E)-Bromoenol lactone) 是一种不可逆的选择性的和有效的钙依赖性磷脂酶 A2 (iPLA2β) 抑制剂，其 IC50 值约为 7 μM，可抑制抗原刺激的肥大细胞胞吐作用，而不会阻止 Ca2+ 的大量涌入。

Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx.

In RBL 2H3 and bone marrow-derived mast cells (BMMCs), Ca2+ entry is critical for exocytosis. Bromoenol lactone inhibits exocytosis when stimulated using a Ca2+ ionophore A23187, which passively transports Ca2+ down a concentration gradient and also in permeabilised mast cells where Ca2+ entry is no longer relevant. Moreover, Bromoenol lactone has only a minor effect on antigen- or thapsigargin-stimulated Ca2+ signalling, both the release from internal stores and sustained elevation due to Ca2+ influx.

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Metabolic Enzyme/Protease

Phospholipase

Phospholipase

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88070-98-8

317.18

C16H13BrO2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (157.64 mM; 超声助溶 )

O=C1C(C=2C3=C(C=CC2)C=CC=C3)CC/C(=C\Br)/O1

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(-20℃)

With Ice Pack

≥ 2 years